Cancer has become one of the major reasons for disease mortality with drastic increase of death rate in recent years. The reason for most of these deaths is due to the inefficacy and failure of the current methods of treatments or due to the unavailability of treatment options. Even after extensive research that has been carried out in the field, there is no gold standard in cancer therapy. With the advancement of the field of nanomedicine and materials science, many research works are being aimed at developing micro and nanocarriers for site-specific delivery of anticancer drugs. As a further advancement in the field, smart carriers, based on nanobiomaterials, which respond to various external and internal stimuli and act locally are being developed to improve the efficacy of current treatments. These smart nanobiomaterials act as carriers for not only anticancer drugs but also for gene and other biomolecules. Keeping the importance and advancement of smart carrier anticancer drug delivery system (AcDDS) in view, this review focuses on stimuli responsive nanobiomaterials that are currently being studied for cancer therapy. Copyright © 2014 American Scientific Publishers.